1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Rociletinib

Rociletinib  (Synonyms: CO-1686; AVL-301; CNX-419)

Cat. No.: HY-15729 Purity: 99.79%
COA Handling Instructions

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

For research use only. We do not sell to patients.

Rociletinib Chemical Structure

Rociletinib Chemical Structure

CAS No. : 1374640-70-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
50 mg USD 165 In-stock
100 mg USD 275 In-stock
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Rociletinib:

Top Publications Citing Use of Products

    Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811.  [Abstract]

    Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

    Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811.  [Abstract]

    The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 µmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

    IC50 & Target

    EGFRL858R/T790M

    21.5 nM (Ki)

    EGFRT790M

    303.3 nM (Ki)

    In Vitro

    Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    555.55

    Formula

    C27H28F3N7O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (225.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8000 mL 9.0001 mL 18.0002 mL
    5 mM 0.3600 mL 1.8000 mL 3.6000 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.79%

    References
    Cell Assay
    [1]

    Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI50) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×107 tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm3, Animals are dosed with compounds (Rociletinib) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib (CO-1686)) is initiated at a mean tumor size of approximately 160 mm3. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm3. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8000 mL 9.0001 mL 18.0002 mL 45.0005 mL
    5 mM 0.3600 mL 1.8000 mL 3.6000 mL 9.0001 mL
    10 mM 0.1800 mL 0.9000 mL 1.8000 mL 4.5000 mL
    15 mM 0.1200 mL 0.6000 mL 1.2000 mL 3.0000 mL
    20 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2500 mL
    25 mM 0.0720 mL 0.3600 mL 0.7200 mL 1.8000 mL
    30 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5000 mL
    40 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1250 mL
    50 mM 0.0360 mL 0.1800 mL 0.3600 mL 0.9000 mL
    60 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7500 mL
    80 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5625 mL
    100 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4500 mL
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    Rociletinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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